Drug-Linker Conjugates for ADC

Deruxtecan is an ADC drug-linker conjugate composed of a derivative of DX-8951 (DXd) and a maleimide-GGFG peptide linker used in the synthesis of DS-8201 and U3-1402.

Vipivotide tetraxetan (PSMA-617) is a highly potent inhibitor of prostate-specific membrane antigen (PSMA) with a Ki of 0.37 nM.

VCMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate for ADC with potent antitumor activity.

SMCC-DM1 is a drug-coupler coupler consisting of a potent microtubule disrupter, DM1, and a coupler, SMCC, for the preparation of antibody-drug couplers.

Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) is a drug-linker conjugate for ADC. Mc-MMAE is a maleimidocaproyl-conjugated monomethyl auristatin E, which is a potent tubulin inhibitor.

Fmoc-Val-Cit-PAB-MMAE is consisted of the ADCs linker (Fmoc-Val-Cit-PAB) and potent tubulin inhibitor (MMAE). Fmoc-Val-Cit-PAB-MMAE is a drug-linker conjugate for ADC.

McMMAF is a protective group-conjugated MMAF. MMAF is a potent tubulin polymerization inhibitor.It is a MMAF derivative having a Maleimidocaproyl linker (MC linker), which is ready to conjugate to antibody or other proteins or biopolymers. Mafodotin is a useful agent for make antibody drug conjugate (ADC) for targeted drug delivery.

Mc-VC-PAB-SN38 consists of a cleavable ADC linker (Mc-VC-PAB) and SN38, which is part of an antibody-coupled reactive molecule commonly used to synthesize antibody-coupled reactive molecules (ADCs) that target sites of action.

CL2A-SN-38 consists of a CL2A linker and an anticancer compound, SN-38, which delivers active molecules within tumor cells and in the tumor microenvironment, often in conjunction with antibodies to make biologically active antibody-coupled reactive molecules (ADCs).

Lys-SMCC-DM1 (Lys-Nε-MCC-DM1) is an antibody-drug conjugate (ADC) targeting human epidermal growth factor receptor 2 (HER2). It contains the microtubule polymerization inhibitor DM1 as the active metabolite, which inhibits microtubule polymerization. It is commonly used in breast cancer research.

Vc-MMAD, a drug-linker conjugate for Antibody-Drug Conjugates (ADCs), combines the ADC linker Val-Cit (Valine-Citrulline) with the potent tubulin inhibitor MMAD. This compound leverages the targeting capability of ADCs to deliver the cytotoxic agent MMAD specifically to cancer cells, enhancing therapeutic efficacy while minimizing off-target effects.

Val-Cit-PAB-MMAE is a drug-linker conjugate for ADC. Val-Cit-PAB-MMAE contains the ADCs linker (peptide Val-Cit-PAB) and a potent tubulin inhibitor MMAE . MMAE a potent mitotic inhibitor by inhibiting tubulin polymerization[1].

PSMA-ALB-56 is a PSMA-targeting radioactive ligand with antitumor activity, composed of glutamic urea PSMA binding entities, DOTA chelating agents, and albumin binders based on 4-(p-iodophenyl)- fragment or p(tolyl)- fragment.

DGN549-L is a DNA alkylator that enables antibody conjugation at lysine residues, making it ideal for antibody-drug conjugate (ADC) synthesis.

MC-GGFG-DX8951 (MC-GGFG-Exatecan) is an antibody-coupled drug (ADC) drug-linker conjugate (DLC) consisting of DX8951, a potent DNA topoisomerase I inhibitor, the linker MC, and the cleavable peptide chain GGFG, and has antitumor potential.

MC-DM1 is a drug-linker conjugate composed of a potent microtubule-disrupting agent DM1 and a linker MC to make antibody drug conjugate (ADC).

SuO-Glu-Val-Cit-PAB-MMAE is a chemical compound consisting of a cleavable ADC linker (SuO-Glu-Val-Cit-PAB) and a potent tubulin inhibitor (MMAE). It is employed in the synthesis of antibody-drug conjugates (ADCs).

MP-PEG4-Val-Lys-Gly-7-MAD-MDCPT is a Camptothecin-linker and a drug-linker conjugate for antibody-drug conjugate (ADC).

TLR7 8 agonist 4 hydroxy-PEG10-acid [compound 9] is a drug-linker conjugate used in antibody-drug conjugates (ADC), exhibiting remarkable antitumor activity. It utilizes TLR7 8 agonist 4, a potent activator of TLR7 8, linked to hydroxy-PEG10-acid via a cleavable bond, demonstrating promising pharmaceutical potential in ADC-based therapeutics.

Azido-PEG4-Val-Cit-PAB-MMAE is a drug-linker conjugate for antibody-drug conjugates (ADCs), incorporating the tubulin inhibitor monomethyl auristatin E (MMAE) and linked via the cleavable Azido-PEG4-Val-Cit-PAB-OH.

Mal-PEG4-VC-PAB-DMEA-PNU-159682 is a drug-linker conjugate designed for antibody-drug conjugate (ADC) therapy. It combines the ADC linker, Mal-PEG4-VC-PAB, with the potent ADC cytotoxin, DMEA-PNU-159682. The cytotoxin, DMEA-PNU-159682, is derived from metabolites of nemorubicin (MMDX) found in liver microsomes, as well as the ADC cytotoxin PNU-159682 [1].

Mal-C2-Gly3-EDA-PNU-159682, a drug-linker conjugate for antibody-drug conjugates (ADC), integrates the cleavable ADC linker Mal-C2-Gly3-EDA with the potent cytotoxin PNU-159682.

SPB is a potent anti-inflammatory drug-linker conjugate for Antibody-Drug Conjugates (ADC), utilizing Xanthotoxol connected through the ADC linker.

MC-Alkyl-Hydrazine Modified MMAF is a potent antitumor drug-linker conjugate for ADC, utilizing Modified MMAF, a tubulin inhibitor, connected via a noncleavable MC-Alkyl-Hydrazine linkage[1].

MC-Val-Cit-PAB-Auristatin E is an antibody-drug conjugate (ADC) linker compound with Auristatin E, a potent cytotoxic tubulin modifier, attached via the MC-Val-Cit-PAB linker, demonstrating significant antitumor activity.

SC-VC-PAB-MMAE is a potent antitumor drug-linker conjugate for antibody-drug conjugates (ADCs), consisting of the anti-mitotic agent monomethyl auristatin E (MMAE, a tubulin inhibitor) linked via the cleavable linker SC-VC-PAB[1].

Mal-C6-α-Amanitin, an ADC (antibody-drug conjugate) linker drug, incorporates the powerful antitumor agent α-Amanitin, an inhibitor of RNA polymerase II, through the Mal-C6 linker, showcasing potent antitumor activity.

MC-VC-PABC-Aur0101 is a potent anticancer drug-linker conjugate for Antibody-Drug Conjugates (ADCs), incorporating Aur0101, an auristatin microtubule inhibitor, linked via the MC-VC-PABC linker to boost antitumor efficacy.

Daunorubicinol, a potent antitumor drug-linker conjugate for antibody-drug conjugate (ADC) applications, utilizes Aur0101 (DNA Topoisomerase II inhibitor) connected through the ADC linker[1].

MC-Sq-Cit-PAB-Gefitinib is a potent antitumor drug-linker conjugate for Antibody-Drug Conjugates (ADC), utilizing Gefitinib—an EGFR tyrosine kinase inhibitor—connected through the MC-Sq-Cit-PAB ADC linker.

AcLys-PABC-VC-Aur0101 is a drug-linker conjugate for anti-CXCR4 ADC, exhibiting potent antitumor activity and comprising the auristatin microtubule inhibitor Aur0101, connected through the cleavable linker AcLys-PABC-VC[1].

Mal-PEG8-amide-Val-Ala-(4-NH2)-Exatecan is a conjugated compound used in the synthesis of antibody-drug conjugates (ADCs), featuring a topoisomerase inhibitor derivative linked via a linker to a specific ligand unit[1].

β-Glucuronide-dPBD-PEG5-NH2 TFA is a β-glucuronide-linked pyrrolobenzodiazepine dimer used in the synthesis of the antibody-drug conjugate (ADC) cIRCR201-dPBD, employing a cleavable β-glucuronide linkage. It serves as a proagent to reduce side effects, induce apoptosis, and arrest the cell cycle, exhibiting antitumor activity [1].

Deruxtecan (1R) is a drug-linker conjugate for antibody-drug conjugates (ADC) [1].

Glucocorticoid receptor agonist-1 Ala-Ala-Mal (compound 88), a glucocorticosteroid and glucocorticoid receptor agonist, can be conjugated with Adalimumab to formulate an ADC [1].

OH-Glu-Val-Cit-PAB-MMAE is a compound consisting of a cleavable ADC linker (OH-Glu-Val-Cit-PAB) and a potent tubulin inhibitor (MMAE), used in the synthesis of antibody-drug conjugates (ADCs) [1].

Azide-PEG4-VC-PAB-Doxorubicin is an agent-linker conjugate used in antibody-drug conjugate (ADC) applications, comprising the cytotoxic anthracycline antibiotic Doxorubicin linked through the Azide-PEG4-VC-PAB linker [1].

Mc-Val-Cit-PAB-Gefitinib chloride is a conjugate agent-linker for antibody-drug conjugates (ADCs) that combines Gefitinib, an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, with the proprietary ADC linker Mc-Val-Cit-PAB [1].

Mal-PEG8-Val-Cit-PAB-MMAF, a drug-linker conjugate utilized for antibody-drug conjugates (ADCs), includes a cleavable linker system and the potent tubulin inhibitor monomethyl auristatin F (MMAF), designed for targeted cancer therapy.

CL2E-SN-38 TFA, a structurally stable and highly releasable antibody drug conjugate (ADC), comprises SN-38, the active metabolite of Irinotecan derived from camptothecins, known for its Topoisomerase I inhibitory activity [1].

MC-VC-PAB-MMAD is a conjugate for antibody-drug conjugates (ADCs) that exhibits potent antitumor activity by employing MMAD, a powerful tubulin inhibitor, connected through the cleavable ADC linker MC-VC-PAB [1].

Vc-seco-DUBA is a drug-linker conjugate for ADC with potent antitumor activity by using DUBA (DNA alkylating agent), linked via the ADC linker Vc-seco[1].

MC-VC-PABC-C6-alpha-Amanitin is an antibody-drug conjugate that combines the anticancer toxin alpha-Amanitin with the monoclonal antibody MC-VC-PABC-C6. Alpha-Amanitin, a potent inhibitor of RNA polymerase IIα, enables the conjugate to selectively target and recognize HER2-positive tumor cells, making it a valuable research tool in the study of breast and gastric cancers [1].

MC-Gly-Gly-Phe-Gly-GABA-Exatecan, functioning both as an ADC linker agent and a topoisomerase inhibitor (Exatecan), displays cytotoxic and antitumor properties in vitro and in vivo [1] [2]. It specifically targets various antibodies and boasts an IC 50 of 22 μM.

MC-GGFG-(7ethanol-10NH2-11F-Camptothecin) (compound 141) is a protease-cleavable drug-linker conjugate utilized in antibody-drug conjugates (ADCs), featuring an MC-GGFG linker that allows for enzymatic cleavage [1].

Mal-cyclohexane-Gly-Gly-Phe-Gly-Exatecan is a linker molecule utilized in the synthesis of antibody-drug conjugates (ADCs), exhibiting potent antitumor activity in vitro and in vivo [1].

Glucocorticoid Receptor Agonist-4 Ala-Ala-Mal (Compound Preparation 9) is a conjugate of anti-human TNFα antibody and glucocorticoid receptor agonist (GC). It is applicable in the research of autoimmune and inflammatory diseases [1].

SMP-33693 is an Antibody-Drug Conjugate (ADC) known for its low payload shedding rate and demonstrated in vivo tumor inhibition in ovarian, gastric, and breast cancers [1].